Results 21 to 30 of about 766,676 (298)
Cholestasis is a common clinical disease caused by a disorder in bile acids (BAs) homeostasis, which promotes its development. The Farnesoid X receptor (FXR) plays a critical role in regulating BAs homeostasis, making it an essential target for ...
Lili Xi +5 more
doaj +1 more source
A–C Estrogens as Potent and Selective Estrogen Receptor-Beta Agonists (SERBAs) to Enhance Memory Consolidation under Low-Estrogen Conditions [PDF]
Estrogen receptor-beta (ERβ) is a drug target for memory consolidation in postmenopausal women. Herein is reported a series of potent and selective ERβ agonists (SERBAs) with in vivo efficacy that are A–C estrogens, lacking the B and D estrogen rings ...
Donaldson, William A. +12 more
core +4 more sources
Immune Checkpoints as Therapeutic Targets in Autoimmunity
Antibodies that block the immune checkpoint receptors PD1 and CTLA4 have revolutionized the treatment of melanoma and several other cancers, but in the process, a new class of drug side effect has emerged—immune related adverse events.
Christopher Paluch +9 more
doaj +1 more source
The extracellular domain of tumor necrosis factor receptors (TNFR) generally require assembly into a homotrimeric quaternary structure as a prerequisite for initiation of signaling via the cytoplasmic domains.
George Fromm +2 more
doaj +1 more source
Down Regulation with Luteal GnRH Agonist Therapy in Euploid Embryo Transfers Does Not Impact Pregnancy Rates [PDF]
Introduction : Gonadotropin-releasing hormone (GnRH) agonists have been used during assisted reproductive technology (ART) treatment for pituitary suppression and stimulation.
Bergin, MD, Keri +4 more
core +1 more source
Orexin-Corticotropin-Releasing Factor Receptor Heteromers in the Ventral Tegmental Area as Targets for Cocaine [PDF]
Release of the neuropeptides corticotropin-releasing factor (CRF) and orexin-A in the ventral tegmental area (VTA) play an important role in stress-induced cocaine-seeking behavior.
Aguinaga, David +17 more
core +1 more source
Phlorotannins are polyphenolic compounds in marine alga, especially the brown algae. Among numerous phlorotannins, dieckol and phlorofucofuroeckol-A (PFF-A) are the major ones and despite a wider biological activity profile, knowledge of the G protein ...
Pradeep Paudel +5 more
doaj +1 more source
Identification of Two Novel α1-AR Agonists Using a High-Throughput Screening Model
α1-Adrenoceptors (ARs; 1A, 1B, and 1D) have been determined to perform different prominent functions in the physiological responses of the sympathetic nervous system.
Fang Xu +7 more
doaj +1 more source
ALIX binds a YPX(3)L motif of the GPCR PAR1 and mediates ubiquitin-independent ESCRT-III/MVB sorting. [PDF]
The sorting of signaling receptors to lysosomes is an essential regulatory process in mammalian cells. During degradation, receptors are modified with ubiquitin and sorted by endosomal sorting complex required for transport (ESCRT)-0, -I, -II, and -III ...
Chen, Buxin +7 more
core +3 more sources
We are developing an orally available small molecule, allosteric TSH receptor (TSHR) agonist for follow up diagnostics of patients with thyroid cancer.
Susanne Neumann +7 more
doaj +1 more source

